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MedKoo Cat#: 329444 | Name: Traxoprodil
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Traxoprodil, also known as CP-101606 and CP 98113, is a NR2B N-Methyl-D-Aspartate (NMDA) antagonist potentially for the treatment of major depressive. Traxoprodil potentiates the antidepressant-like effects of certain antidepressant drugs in the forced swim test in mice. Traxoprodil decreases pentylenetetrazol-induced seizures.

Chemical Structure

Traxoprodil
Traxoprodil
CAS#134234-12-1 (free base)

Theoretical Analysis

MedKoo Cat#: 329444

Name: Traxoprodil

CAS#: 134234-12-1 (free base)

Chemical Formula: C20H25NO3

Exact Mass: 327.1834

Molecular Weight: 327.42

Elemental Analysis: C, 73.37; H, 7.70; N, 4.28; O, 14.66

Price and Availability

Size Price Availability Quantity
10mg USD 250.00
25mg USD 440.00 2 Weeks
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Related CAS #
134234-12-1 (free base) 188591-67-5 (mesylate)
Synonym
Traxoprodil; CP-101606; CP101606; CP 101606; CP 98113.
IUPAC/Chemical Name
1-((1S,2S)-1-hydroxy-1-(4-hydroxyphenyl)propan-2-yl)-4-phenylpiperidin-4-ol
InChi Key
QEMSVZNTSXPFJA-HNAYVOBHSA-N
InChi Code
InChI=1S/C20H25NO3/c1-15(19(23)16-7-9-18(22)10-8-16)21-13-11-20(24,12-14-21)17-5-3-2-4-6-17/h2-10,15,19,22-24H,11-14H2,1H3/t15-,19+/m0/s1
SMILES Code
O[C@@H](C1=CC=C(O)C=C1)[C@H](C)N2CCC(C3=CC=CC=C3)(O)CC2
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Related CAS# 134234-12-1 (Traxoprodil free base) 189894-57-3 (Traxoprodil mesylate hydrate)

Preparing Stock Solutions

The following data is based on the product molecular weight 327.42 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Ye S, Han Y, Wei Z, Li J. Binding Affinity and Mechanisms of Potential Antidepressants Targeting Human NMDA Receptors. Molecules. 2023 May 25;28(11):4346. doi: 10.3390/molecules28114346. PMID: 37298821; PMCID: PMC10254814. 2: Wang Y, Liang Z, Song W, Qin Y, Todd N, Gao M. Traxoprodil Produces Antidepressant-Like Behaviors in Chronic Unpredictable Mild Stress Mice through BDNF/ERK/CREB and AKT/FOXO/Bim Signaling Pathway. Oxid Med Cell Longev. 2023 Feb 10;2023:1131422. doi: 10.1155/2023/1131422. PMID: 36819781; PMCID: PMC9937761. 3: Qin Y, Guo X, Song W, Liang Z, Wang Y, Feng D, Yang Y, Li M, Gao M. Antidepressant-like effect of CP-101,606: Evidence of mTOR pathway activation. Mol Cell Neurosci. 2023 Mar;124:103821. doi: 10.1016/j.mcn.2023.103821. Epub 2023 Feb 10. PMID: 36775184. 4: Haduch A, Bromek E, Pukło R, Jastrzębska J, Danek PJ, Daniel WA. The Effect of the Selective N-methyl-D-aspartate (NMDA) Receptor GluN2B Subunit Antagonist CP-101,606 on Cytochrome P450 2D (CYP2D) Expression and Activity in the Rat Liver and Brain. Int J Mol Sci. 2022 Nov 8;23(22):13746. doi: 10.3390/ijms232213746. PMID: 36430225; PMCID: PMC9691159. 5: Khormali M, Heidari S, Ahmadi S, Arab Bafrani M, Baigi V, Sharif-Alhoseini M. N-methyl-D-aspartate receptor antagonists in improving cognitive deficits following traumatic brain injury: a systematic review. Brain Inj. 2022 Jul 29;36(9):1071-1088. doi: 10.1080/02699052.2022.2109749. Epub 2022 Aug 23. PMID: 35997315. 6: Vasiliu O. Investigational Drugs for the Treatment of Depression (Part 2): Glutamatergic, Cholinergic, Sestrin Modulators, and Other Agents. Front Pharmacol. 2022 Jun 17;13:884155. doi: 10.3389/fphar.2022.884155. PMID: 35847011; PMCID: PMC9284317. 7: Shin EJ, Nguyen BT, Jeong JH, Hoai Nguyen BC, Tran NKC, Sharma N, Kim DJ, Nah SY, Lichtstein D, Nabeshima T, Kim HC. Ouabain inhibitor rostafuroxin attenuates dextromethorphan-induced manic potential. Food Chem Toxicol. 2021 Dec;158:112657. doi: 10.1016/j.fct.2021.112657. Epub 2021 Nov 3. PMID: 34740715. 8: Smaga I, Wydra K, Suder A, Sanak M, Caffino L, Fumagalli F, Filip M. Enhancement of the GluN2B subunit of glutamatergic NMDA receptors in rat brain areas after cocaine abstinence. J Psychopharmacol. 2021 Oct;35(10):1226-1239. doi: 10.1177/02698811211048283. Epub 2021 Sep 29. PMID: 34587833. 9: Ahnaou A, Heleven K, Biermans R, Manyakov NV, Drinkenburg WH. NMDARs Containing NR2B Subunit Do Not Contribute to the LTP Form of Hippocampal Plasticity: In Vivo Pharmacological Evidence in Rats. Int J Mol Sci. 2021 Aug 12;22(16):8672. doi: 10.3390/ijms22168672. PMID: 34445376; PMCID: PMC8395520. 10: Henter ID, Park LT, Zarate CA Jr. Novel Glutamatergic Modulators for the Treatment of Mood Disorders: Current Status. CNS Drugs. 2021 May;35(5):527-543. doi: 10.1007/s40263-021-00816-x. Epub 2021 Apr 26. PMID: 33904154; PMCID: PMC8201267. 11: Raith H, Schuelert N, Duveau V, Roucard C, Plano A, Dorner-Ciossek C, Ferger B. Differential effects of traxoprodil and S-ketamine on quantitative EEG and auditory event-related potentials as translational biomarkers in preclinical trials in rats and mice. Neuropharmacology. 2020 Jul;171:108072. doi: 10.1016/j.neuropharm.2020.108072. Epub 2020 Mar 31. PMID: 32243874. 12: Becker R, Gass N, Kußmaul L, Schmid B, Scheuerer S, Schnell D, Dorner- Ciossek C, Weber-Fahr W, Sartorius A. NMDA receptor antagonists traxoprodil and lanicemine improve hippocampal-prefrontal coupling and reward-related networks in rats. Psychopharmacology (Berl). 2019 Dec;236(12):3451-3463. doi: 10.1007/s00213-019-05310-3. Epub 2019 Jul 2. PMID: 31267156. 13: Fasipe OJ. The emergence of new antidepressants for clinical use: Agomelatine paradox versus other novel agents. IBRO Rep. 2019 Jan 9;6:95-110. doi: 10.1016/j.ibror.2019.01.001. PMID: 31211282; PMCID: PMC6562183. 14: Wilkinson ST, Sanacora G. A new generation of antidepressants: an update on the pharmaceutical pipeline for novel and rapid-acting therapeutics in mood disorders based on glutamate/GABA neurotransmitter systems. Drug Discov Today. 2019 Feb;24(2):606-615. doi: 10.1016/j.drudis.2018.11.007. Epub 2018 Nov 14. PMID: 30447328; PMCID: PMC6397075. 15: Yates JR, Prior NA, Chitwood MR, Day HA, Heidel JR, Hopkins SE, Muncie BT, Paradella-Bradley TA, Sestito AP, Vecchiola AN, Wells EE. Effects of GluN2B-selective antagonists on delay and probability discounting in male rats: Modulation by delay/probability presentation order. Exp Clin Psychopharmacol. 2018 Dec;26(6):525-540. doi: 10.1037/pha0000216. Epub 2018 Jul 23. PMID: 30035577; PMCID: PMC6283694. 16: Henter ID, de Sousa RT, Zarate CA Jr. Glutamatergic Modulators in Depression. Harv Rev Psychiatry. 2018 Nov/Dec;26(6):307-319. doi: 10.1097/HRP.0000000000000183. PMID: 29465478; PMCID: PMC6102095. 17: Tang H, Kukral D, Li YW, Fronheiser M, Malone H, Pena A, Pieschl R, Sidik K, Tobon G, Chow PL, Bristow LJ, Hayes W, Luo F. Mapping the central effects of (±)-ketamine and traxoprodil using pharmacological magnetic resonance imaging in awake rats. J Psychopharmacol. 2018 Feb;32(2):146-155. doi: 10.1177/0269881117746901. Epub 2018 Jan 30. PMID: 29378483. 18: Tran HQ, Chung YH, Shin EJ, Tran TV, Jeong JH, Jang CG, Nah SY, Yamada K, Nabeshima T, Kim HC. MK-801, but not naloxone, attenuates high-dose dextromethorphan-induced convulsive behavior: Possible involvement of the GluN2B receptor. Toxicol Appl Pharmacol. 2017 Nov 1;334:158-166. doi: 10.1016/j.taap.2017.09.010. Epub 2017 Sep 13. PMID: 28916251. 19: Stasiuk W, Szopa A, Serefko A, Wyska E, Świąder K, Dudka J, Wlaź P, Poleszak E. Influence of the selective antagonist of the NR2B subunit of the NMDA receptor, traxoprodil, on the antidepressant-like activity of desipramine, paroxetine, milnacipran, and bupropion in mice. J Neural Transm (Vienna). 2017 Mar;124(3):387-396. doi: 10.1007/s00702-016-1657-8. Epub 2016 Nov 29. PMID: 27900470; PMCID: PMC5310560. 20: DePoy LM, Zimmermann KS, Marvar PJ, Gourley SL. Induction and Blockade of Adolescent Cocaine-Induced Habits. Biol Psychiatry. 2017 Apr 1;81(7):595-605. doi: 10.1016/j.biopsych.2016.09.023. Epub 2016 Oct 6. PMID: 27871669; PMCID: PMC5359769.